title: Dissolution enhancement of cefdinir with hydroxypropyl-β-cyclodextrin.
abstract: The solid state properties and dissolution behavior of binary systems of cefdinir (CEF) with hydroxypropyl-β-cyclodextrin (HP-β-CD) were investigated. CEF-HP-β-CD interaction in the solution state was studied by phase-solubility analysis and demonstrates the ability of HP-β-CD to complex with CEF giving A(L) type profile with 65.28 ± 1.3 M⁻¹ stability constant. The freeze drying technique was adopted to prepare binary systems of CEF with HP-β-CD in 1:1 molar ratio. The solid inclusion was characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRD), and scanning electron microscopy (SEM). Aqueous solubility of CEF-HP-β-CD inclusion complex was 2.36-fold of pure CEF. The dissolution profiles of inclusion complexes were determined and compared with those of CEF alone and their physical mixtures. The dissolution rate of inclusion complex was superior than the CEF alone. These approaches indicated that CEF was able to form an inclusion complex with HP-β-CD, and the inclusion compounds exhibited different spectroscopic features and properties.
authors.affiliation: School of pharmacy, Guangdong Pharmaceutical University , Guangzhou , PR China.
authors.forename: Bohong
authors.initials: B
authors.lastname: Guo
authors.forename: Shufen
authors.initials: S
authors.lastname: Zhong
authors.forename: Niying
authors.initials: N
authors.lastname: Li
authors.forename: Xiaofang
authors.initials: X
authors.lastname: Li
authors.forename: Jun
authors.initials: J
authors.lastname: Yi
authors.forename: Miaozhen
authors.initials: M
authors.lastname: Jin
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D000077525:Cefdinir; D002511:Cephalosporins / Q000737:chemistry*; D055598:Chemical Phenomena; D004339:Drug Compounding; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D005612:Freeze Drying; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D044367:Phase Transition; D033362:Powder Diffraction; D064449:Sequestering Agents / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D005079:Excipients; D064449:Sequestering Agents; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000077525:Cefdinir